Abstract
Neuropeptides play crucial, mediatory roles in many processes that occur in both CNS and PNS. The commonly accepted dogma for the release of bioactive peptides involves cleavage of inactive precursor by sequential action of proteinases recognizing dibasic stretches, followed by truncation of C-terminal Arg/Lys by the carboxypeptidase-like enzyme(s). Dynorphin convertases play an important role in CNS by regulating dynorphins level and also releasing enkephalins, thus maintaining a balance between these neuropeptides and their distinct functions (dynorphins are preferentially bound to kappa receptors and enkephalins are directed toward delta receptors). Knowledge on the cleavage fragments of dynorphins is important for understanding the pharmacological activity of these peptides. As some new data emerged in the literature, we would like to update recent achievements and progress concerning functions of such convertases, inhibitors, and their potential role in future pharmacotherapy.
Keywords: Dynorphins, conversion, inhibitors, pharmacology, enzymes, neuropeptides.
Current Pharmaceutical Design
Title:Dynorphin Convertases and their Functions in CNS
Volume: 19 Issue: 6
Author(s): Joanna Ner and Jerzy Silberring
Affiliation:
Keywords: Dynorphins, conversion, inhibitors, pharmacology, enzymes, neuropeptides.
Abstract: Neuropeptides play crucial, mediatory roles in many processes that occur in both CNS and PNS. The commonly accepted dogma for the release of bioactive peptides involves cleavage of inactive precursor by sequential action of proteinases recognizing dibasic stretches, followed by truncation of C-terminal Arg/Lys by the carboxypeptidase-like enzyme(s). Dynorphin convertases play an important role in CNS by regulating dynorphins level and also releasing enkephalins, thus maintaining a balance between these neuropeptides and their distinct functions (dynorphins are preferentially bound to kappa receptors and enkephalins are directed toward delta receptors). Knowledge on the cleavage fragments of dynorphins is important for understanding the pharmacological activity of these peptides. As some new data emerged in the literature, we would like to update recent achievements and progress concerning functions of such convertases, inhibitors, and their potential role in future pharmacotherapy.
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Cite this article as:
Ner Joanna and Silberring Jerzy, Dynorphin Convertases and their Functions in CNS, Current Pharmaceutical Design 2013; 19 (6) . https://dx.doi.org/10.2174/1381612811319060006
DOI https://dx.doi.org/10.2174/1381612811319060006 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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